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Featured researches published by Matthias Schaefer.
Hypertension | 2009
Matthias Löhn; Oliver Plettenburg; Yuri Ivashchenko; Aimo Kannt; Armin Hofmeister; Dieter Kadereit; Matthias Schaefer; Wolfgang Linz; Markus Kohlmann; Jean-Marc Herbert; Philip Janiak; Stephen E. O'Connor; Hartmut Ruetten
Abstract—Recent advances in basic and clinical research have identified Rho kinase as an important target potentially implicated in a variety of cardiovascular diseases. Rho kinase is a downstream mediator of RhoA that leads to stress fiber formation, membrane ruffling, smooth muscle contraction, and cell motility. Increased Rho-kinase activity is associated with vasoconstriction and elevated blood pressure. We identified a novel inhibitor of Rho kinase (SAR407899) and characterized its effects in biochemical, cellular, tissue-based, and in vivo assays. SAR407899 is an ATP-competitive Rho-kinase inhibitor, equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. It is highly selective in panel of 117 receptor and enzyme targets. SAR407899 is ≈8-fold more active than fasudil. In vitro, SAR407899 demonstrated concentration-dependent inhibition of Rho-kinase-mediated phosphorylation of myosin phosphatase, thrombin-induced stress fiber formation, platelet-derived growth factor-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 potently (mean IC50 values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. In vivo, over the dose range 3 to 30 mg/kg PO, SAR407899 lowered blood pressure in a variety of rodent models of arterial hypertension. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632. In conclusion, SAR407899 is a novel and potent selective Rho-kinase inhibitor with promising antihypertensive activity.
Archive | 2013
Matthias Schaefer; Josef Pernerstorfer; Dieter Kadereit; Hartmut Strobel; Werngard Czechtizky; L. Charlie Chen; Alena Safarova; Aleksandra Weichsel; Marcel Patek
Archive | 2009
Dieter Kadereit; Matthias Schaefer; Werngard Czechtizky
Archive | 2011
Dieter Kadereit; Matthias Schaefer; Stephanie Hachtel; Axel Dietrich; Thomas Huebschle; Katrin Hiss
Archive | 2011
Dieter Kadereit; Matthias Schaefer; Stephanie Hachtel; Axel Dietrich; Thomas Huebschle; Katrin Hiss
Archive | 2012
Dieter Kadereit; Matthias Schaefer; Stephanie Hachtel; Thomas Huebschle; Katrin Hiss
Archive | 2011
Dieter Kadereit; Matthias Schaefer; Stephanie Hachtel; Axel Dietrich; Thomas Huebschle; Andreas Gille; Katrin Hiss
Archive | 2012
Dieter Kadereit; Matthias Schaefer; Stephanie Hachtel; Thomas Huebschle; Katrin Hiss; Silke Haag-diergarten
Archive | 2017
Matthias Schaefer; Wolfgang Linz
Archive | 2016
Matthias Schaefer; Josef Pernerstorfer; Dieter Kadereit; Hartmut Strobel; Werngard Czechtizky; Charlie Chen L; Alena Safarova; Aleksandra Weichsel; Marcel Patek